Practical Fragments

It’s been a couple years since Practical Fragments last updated our “fragments in the clinic” list . Before doing so it makes sense to high...

As our poll last year demonstrated, there is no shortage of methods to find fragments. But that doesn’t mean new approaches aren’t welcome,...

Three years ago we discussed using DNA-encoded libraries to find and link fragments. In a new open-access Bioorg. Med. Chem. article , Nic...

Anyone who has spent much time in drug discovery will have been asked what they've done to cure the common cold. In a paper just publis...

Mycobacterium tuberculosis (Mtb) , the cause of its eponymous disease, is making an unwelcome comeback. Current treatments are lengthy, an...

One of the more exciting phenomena in fragment-based approaches is synergy (or superadditivity), in which the binding energy of linked fra...

The strategy of fragment linking dates to the origins of fragment-based lead discovery. The idea that two low affinity binders can be linke...

Linking two fragments together to achieve a boost in potency has been done a number of times (see here , here , here , and here ), though it...

Fragment linking is one of the most seductive forms of fragment-based lead discovery: take two low-affinity binders, link them together, and...

Fragment linking is a topic we’ve discussed a few times . One of its great appeals is that, all other things being equal, the entropic cost...

In the world of fragment-based ligand discovery, researchers hope that two fragments, when linked together, will behave at least additively:...